Tanzisertib

CAS号

899805-25-5

分子式

C21H23F3N6O2

主要靶点

JNK

仅限科研使用

Cat No : CM04920

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Synonyms

Tanzisertib|Inhibitor|JNK|JNK2|JNK3|JNK1|inhibit|CC 930|CC930|CC-930



产品信息

CAS号 899805-25-5
分子式 C21H23F3N6O2
主要靶点 JNK
主要通路 MAPK 信号通路
分子量 448.44
纯度 99.28%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Tanzisertib|Inhibitor|JNK|JNK2|JNK3|JNK1|inhibit|CC 930|CC930|CC-930

靶点活性

JNK1:61 nM|JNK2:7 nM|JNK3:6 nM

体内活性

Tanzisertib (CC-930)(10及30mg/kg,口服)在急性大鼠LPS诱发的TNFa产生PK-PD模型中[1],对TNFa产生的抑制率分别为23%和77%。此外,Tanzisertib (CC-930)(150mg/kg)能防止不同模型中纤维化的发展,并且还可促进已存在纤维化的逆转[3]。

体外活性

Tanzisertib (CC-930) 通过抑制人类PBMC中由phorbol-12-myristate-13-acetate和phytohemeagglutinin刺激产生的phospho-cJun (IC50=1 μM)[1],同时阻断由纤维化细胞因子激活的JNK途径,从而在系统性硬化症中发挥作用[3]。Tanzisertib (CC-930) (1-2 μM) 显著减少了肝细胞的凋亡和坏死,消除了FC负载的WT肝细胞中的凋亡和坏死[2]。

溶解度

DMSO:33 mg/mL (73.59 mM)

参考文献

1.Plantevin Krenitsky V, et al. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.
2.Gan LT, et al. Hepatocyte free cholesterol lipotoxicity results from JNK1-mediated mitochondrial injury and is HMGB1 and TLR4-dependent. J Hepatol. 2014 Dec;61(6):1376-84.
3.Reich N, et al. Jun N-terminal kinase as a potential molecular target for prevention and treatment of dermal fibrosis. Ann Rheum Dis. 2012 May;71(5):737-45.
4.Tavernier SJ, et al. Regulated IRE1-dependent mRNA decay sets the threshold for dendritic cell survival. Nat Cell Biol. 2017 Jun;19(6):698-710.

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